JP2005500351A5 - - Google Patents
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- Publication number
- JP2005500351A5 JP2005500351A5 JP2003517018A JP2003517018A JP2005500351A5 JP 2005500351 A5 JP2005500351 A5 JP 2005500351A5 JP 2003517018 A JP2003517018 A JP 2003517018A JP 2003517018 A JP2003517018 A JP 2003517018A JP 2005500351 A5 JP2005500351 A5 JP 2005500351A5
- Authority
- JP
- Japan
- Prior art keywords
- mixture
- water
- atorvastatin calcium
- crystalline form
- hydrate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 claims 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 14
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 12
- 238000000034 method Methods 0.000 claims 10
- 239000011541 reaction mixture Substances 0.000 claims 10
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 9
- OJRHUICOVVSGSY-RXMQYKEDSA-N (2s)-2-chloro-3-methylbutan-1-ol Chemical compound CC(C)[C@H](Cl)CO OJRHUICOVVSGSY-RXMQYKEDSA-N 0.000 claims 8
- 229960001770 atorvastatin calcium Drugs 0.000 claims 8
- 239000002904 solvent Substances 0.000 claims 8
- 239000003960 organic solvent Substances 0.000 claims 7
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 6
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims 6
- 229960005370 atorvastatin Drugs 0.000 claims 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 6
- -1 aliphatic nitrile Chemical class 0.000 claims 5
- 238000010992 reflux Methods 0.000 claims 5
- GNFTZDOKVXKIBK-UHFFFAOYSA-N 3-(2-methoxyethoxy)benzohydrazide Chemical compound COCCOC1=CC=CC(C(=O)NN)=C1 GNFTZDOKVXKIBK-UHFFFAOYSA-N 0.000 claims 4
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 4
- 238000001914 filtration Methods 0.000 claims 4
- 239000000243 solution Substances 0.000 claims 4
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical group CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- FVSKHRXBFJPNKK-UHFFFAOYSA-N propionitrile Chemical compound CCC#N FVSKHRXBFJPNKK-UHFFFAOYSA-N 0.000 claims 3
- FGUUSXIOTUKUDN-IBGZPJMESA-N C1(=CC=CC=C1)N1C2=C(NC([C@H](C1)NC=1OC(=NN=1)C1=CC=CC=C1)=O)C=CC=C2 Chemical compound C1(=CC=CC=C1)N1C2=C(NC([C@H](C1)NC=1OC(=NN=1)C1=CC=CC=C1)=O)C=CC=C2 FGUUSXIOTUKUDN-IBGZPJMESA-N 0.000 claims 2
- 239000007864 aqueous solution Substances 0.000 claims 2
- 150000002825 nitriles Chemical class 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 238000003756 stirring Methods 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 1
- 229910001854 alkali hydroxide Inorganic materials 0.000 claims 1
- 150000008044 alkali metal hydroxides Chemical class 0.000 claims 1
- 125000005907 alkyl ester group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 150000007860 aryl ester derivatives Chemical class 0.000 claims 1
- 159000000007 calcium salts Chemical class 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- UOENAPUPIPQFOY-UHFFFAOYSA-J dicalcium tetraacetate hydrate Chemical compound O.C(C)(=O)[O-].[Ca+2].[Ca+2].C(C)(=O)[O-].C(C)(=O)[O-].C(C)(=O)[O-] UOENAPUPIPQFOY-UHFFFAOYSA-J 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN620MA2001 | 2001-07-30 | ||
| PCT/US2002/000431 WO2003011826A1 (en) | 2001-07-30 | 2002-01-07 | Crystalline forms vi and vii of atorvastatin calcium |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005500351A JP2005500351A (ja) | 2005-01-06 |
| JP2005500351A5 true JP2005500351A5 (enExample) | 2005-10-27 |
Family
ID=35160889
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003517018A Pending JP2005500351A (ja) | 2001-07-30 | 2002-01-07 | 結晶形態ｖｉおよびｖｉｉのアトルバスタチンカルシウム |
Country Status (19)
| Country | Link |
|---|---|
| EP (2) | EP2292600A1 (enExample) |
| JP (1) | JP2005500351A (enExample) |
| KR (1) | KR20040019043A (enExample) |
| CN (1) | CN100471836C (enExample) |
| AU (1) | AU2002255479B2 (enExample) |
| BG (1) | BG108518A (enExample) |
| BR (1) | BR0211488A (enExample) |
| CA (1) | CA2454500C (enExample) |
| CZ (1) | CZ2004126A3 (enExample) |
| EE (1) | EE200400048A (enExample) |
| HR (1) | HRP20040077A2 (enExample) |
| IL (2) | IL159626A0 (enExample) |
| MX (1) | MXPA04000889A (enExample) |
| NO (1) | NO20040390L (enExample) |
| NZ (1) | NZ530785A (enExample) |
| PL (1) | PL368647A1 (enExample) |
| RU (1) | RU2304139C2 (enExample) |
| WO (1) | WO2003011826A1 (enExample) |
| ZA (1) | ZA200400573B (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7411075B1 (en) | 2000-11-16 | 2008-08-12 | Teva Pharmaceutical Industries Ltd. | Polymorphic form of atorvastatin calcium |
| PL362472A1 (en) * | 2000-11-03 | 2004-11-02 | Teva Pharma | Atorvastatin hemi-calcium form vii |
| US7501450B2 (en) | 2000-11-30 | 2009-03-10 | Teva Pharaceutical Industries Ltd. | Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms |
| IL156055A0 (en) | 2000-11-30 | 2003-12-23 | Teva Pharma | Novel crystal forms of atorvastatin hemi calcium and processes for their preparation as well as novel processes for preparing other forms |
| KR100790766B1 (ko) * | 2000-12-27 | 2008-01-03 | 테바 파마슈티컬 인더스트리즈 리미티드 | 아토르바스타틴의 결정 형태, 이의 제조방법 및 이를 포함하는 약제학적 조성물 |
| WO2003070702A1 (en) * | 2002-02-15 | 2003-08-28 | Teva Pharmaceutical Industries Ltd. | Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation, as well as novel processes for preparing atorvastatin hemi-calcium forms i, viii and ix |
| IL163594A0 (en) | 2002-02-19 | 2005-12-18 | Teva Pharma | Processes for desolvating solvates of atorvastatinhemi-calcium and atorvastatin hemi-calcium essentially free of organic solvent |
| EP1424324A1 (en) * | 2002-11-28 | 2004-06-02 | Teva Pharmaceutical Industries Limited | Crystalline form F of Atorvastatin hemi-calcium salt |
| CA2508871C (en) * | 2002-11-28 | 2008-09-09 | Teva Pharmaceutical Industries Ltd. | Crystalline form f of atorvastatin hemi-calcium salt |
| US20050271717A1 (en) | 2003-06-12 | 2005-12-08 | Alfred Berchielli | Pharmaceutical compositions of atorvastatin |
| US7655692B2 (en) | 2003-06-12 | 2010-02-02 | Pfizer Inc. | Process for forming amorphous atorvastatin |
| SI1727795T1 (sl) | 2004-03-17 | 2012-05-31 | Ranbaxy Lab Ltd | Postopek za pripravo atorvastatin kalcija v amorfni obliki |
| WO2005090301A1 (en) * | 2004-03-17 | 2005-09-29 | Ranbaxy Laboratories Limited | Crystalline form of atorvastatin hemi calcium |
| RU2412191C2 (ru) * | 2004-07-16 | 2011-02-20 | Лек Фармасьютиклз Д.Д. | Продукты окислительной деструкции кальций аторвастатина |
| MX2007000765A (es) * | 2004-07-20 | 2007-03-28 | Warner Lambert Co | Formas cristalinas de sal de calcio del acido (r-(r*, r*))-2- (4-fluorofenil)- beta,gama- dihidroxi-5- (1-metiletil)-3 -fenil-4-((fenilamino) (carbonil)-1ih -pirrol-1- heptanoico (2:1). |
| EP1694685A1 (en) | 2004-09-28 | 2006-08-30 | Teva Pharmaceutical Industries Ltd | Process for preparing forms of atorvastatin calcium substantially free of impurities |
| KR20070067175A (ko) | 2004-10-28 | 2007-06-27 | 워너-램버트 캄파니 엘엘씨 | 무정형 아토르바스타틴 형성 방법 |
| WO2006048894A1 (en) * | 2004-11-05 | 2006-05-11 | Morepen Laboratories Limited | Novel crystalline forms of atorvastatin calcium and processes for preparing them. |
| MX2007014329A (es) * | 2005-12-13 | 2008-03-19 | Teva Pharma | Forma cristalina de hemi-calcio de atorvastatina y procesos para la preparacion de ella. |
| EP2185527A2 (en) * | 2007-07-11 | 2010-05-19 | Actavis Group PTC EHF | Novel polymorph of atorvastatin calcium and use thereof for the preparation of amorphous atorvastatin calcium |
| KR20120011249A (ko) | 2010-07-28 | 2012-02-07 | 주식회사 경보제약 | 아토바스타틴 헤미칼슘염의 신규한 결정형, 이의 수화물, 및 그의 제조방법 |
| CN104983702A (zh) * | 2015-07-23 | 2015-10-21 | 青岛蓝盛洋医药生物科技有限责任公司 | 一种治疗高胆固醇血症的药物阿托伐他汀钙组合物片剂 |
| CN108157405B (zh) * | 2018-02-06 | 2020-10-02 | 上海应用技术大学 | 一种灭蟑螂饵剂及其制备方法和应用 |
| WO2025147589A1 (en) | 2024-01-05 | 2025-07-10 | Osanni Bio, Inc. | Implants, compositions, and methods for treating retinal diseases and disorders |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5149837A (en) | 1988-02-22 | 1992-09-22 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| US5003080A (en) | 1988-02-22 | 1991-03-26 | Warner-Lambert Company | Process for trans-6-(2-(substituted-pyrrol-1-yl)alkyl)pryan-2-one inhibitors of cholesterol synthesis |
| US5124482A (en) | 1988-02-22 | 1992-06-23 | Warner-Lambert Company | Process for trans-6-(2-substituted-pyrrol-1-yl)alkyl)pyran-2-one inhibitors of cholesterol synthesis |
| US5216174A (en) | 1988-02-22 | 1993-06-01 | Warner-Lambert Co. | Process for trans-6-[12-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| US5097045A (en) | 1989-02-01 | 1992-03-17 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| US5245047A (en) | 1988-02-22 | 1993-09-14 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| US5248793A (en) | 1990-10-17 | 1993-09-28 | Warner-Lambert Company | Process for the synthesis of (4R-cis)-1,1-dimethylethyl 6-iodomethyl or 6-(phenyl-substituted)sulfonyloxymethyl-2,2-dimethyl-1,3-dioxane-4-acetate |
| US5103024A (en) | 1990-10-17 | 1992-04-07 | Warner-Lambert Company | Process for the synthesis of (4r-cis)-1,1-dimethylethyl 6-cyanomethyl-2,2-dimethyl-1,3-dioxane-4-acetate |
| US5155251A (en) | 1991-10-11 | 1992-10-13 | Warner-Lambert Company | Process for the synthesis of (5R)-1,1-dimethylethyl-6-cyano-5-hydroxy-3-oxo-hexanoate |
| US5298627A (en) | 1993-03-03 | 1994-03-29 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| IL109570A0 (en) * | 1993-05-17 | 1994-08-26 | Fujisawa Pharmaceutical Co | Guanidine derivatives, pharmaceutical compositions containing the same and processes for the preparation thereof |
| DE69634054T2 (de) * | 1995-07-17 | 2005-12-08 | Warner-Lambert Co. | Kristalline (R-(R*, R*))-2-(4-Fluorophenyl)-β, δ-Dihydroxy-5-(1-Methylethyl)-3-Phenyl-4-((Phenylamino)Carbonyl)-1H-Pyrrol-1-Heptancarbonsäure Hemi Calcium Salz (Atorvastatin) |
| HRP960313B1 (en) * | 1995-07-17 | 2002-08-31 | Warner Lambert Co | Form iii crystalline (r- (r*, r*)-2- (4-fluorophenyl) -beta-delta-hydroxy-5-(1-methylethyl) -3-phenyl-4- ((phenylamino) carbonyl -1h-pyrrole-1-heptanoic acid calcium salt (2:1) |
| US6087511A (en) | 1996-07-16 | 2000-07-11 | Warner-Lambert Company | Process for the production of amorphous [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl )-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid) calcium salt (2:1) |
| US5929156A (en) | 1997-05-02 | 1999-07-27 | J.M. Huber Corporation | Silica product for use in elastomers |
| HU226640B1 (en) | 1999-10-18 | 2009-05-28 | Egis Gyogyszergyar Nyilvanosan | Process for producing amorphous atorvastatin calcium salt |
| SI1535613T1 (sl) | 1999-11-17 | 2010-12-31 | Teva Pharma | Postopek za pripravo polimorfne oblike atorvastatin kalcija |
| PL362472A1 (en) * | 2000-11-03 | 2004-11-02 | Teva Pharma | Atorvastatin hemi-calcium form vii |
| IL155890A0 (en) * | 2000-11-16 | 2003-12-23 | Teva Pharma | HYDROLYSIS OF [R(R*,R*)]-2-(4-FLUOROPHENYL)-beta,delta-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIC ACID ESTERS WITH CALCIUM HYDROXIDE |
| IL156055A0 (en) * | 2000-11-30 | 2003-12-23 | Teva Pharma | Novel crystal forms of atorvastatin hemi calcium and processes for their preparation as well as novel processes for preparing other forms |
| KR100790766B1 (ko) * | 2000-12-27 | 2008-01-03 | 테바 파마슈티컬 인더스트리즈 리미티드 | 아토르바스타틴의 결정 형태, 이의 제조방법 및 이를 포함하는 약제학적 조성물 |
| WO2002057229A1 (en) * | 2001-01-19 | 2002-07-25 | Biocon India Limited | FORM V CRYSTALLINE [R-(R*,R*)]-2-(4-FLUOROPHENYL)-ß,$G(D)-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1- HEPTANOIC ACID HEMI CALCIUM SALT. (ATORVASTATIN) |
-
2002
- 2002-01-07 JP JP2003517018A patent/JP2005500351A/ja active Pending
- 2002-01-07 EE EEP200400048A patent/EE200400048A/xx unknown
- 2002-01-07 CA CA002454500A patent/CA2454500C/en not_active Expired - Fee Related
- 2002-01-07 AU AU2002255479A patent/AU2002255479B2/en not_active Ceased
- 2002-01-07 HR HR20040077A patent/HRP20040077A2/xx not_active Application Discontinuation
- 2002-01-07 WO PCT/US2002/000431 patent/WO2003011826A1/en not_active Ceased
- 2002-01-07 CN CNB028150708A patent/CN100471836C/zh not_active Expired - Fee Related
- 2002-01-07 EP EP10010845A patent/EP2292600A1/en not_active Withdrawn
- 2002-01-07 PL PL02368647A patent/PL368647A1/xx unknown
- 2002-01-07 IL IL15962602A patent/IL159626A0/xx unknown
- 2002-01-07 EP EP02724877A patent/EP1414796A1/en not_active Withdrawn
- 2002-01-07 MX MXPA04000889A patent/MXPA04000889A/es active IP Right Grant
- 2002-01-07 KR KR10-2004-7000093A patent/KR20040019043A/ko not_active Ceased
- 2002-01-07 NZ NZ530785A patent/NZ530785A/en not_active IP Right Cessation
- 2002-01-07 CZ CZ2004126A patent/CZ2004126A3/cs unknown
- 2002-01-07 BR BR0211488-7A patent/BR0211488A/pt not_active Application Discontinuation
- 2002-01-07 RU RU2004103470/04A patent/RU2304139C2/ru not_active IP Right Cessation
-
2003
- 2003-12-29 IL IL159626A patent/IL159626A/en not_active IP Right Cessation
-
2004
- 2004-01-09 BG BG108518A patent/BG108518A/xx unknown
- 2004-01-26 ZA ZA200400573A patent/ZA200400573B/en unknown
- 2004-01-29 NO NO20040390A patent/NO20040390L/no not_active Application Discontinuation
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